| 名称 | IC-87114 |
| 描述 | IC-87114 is a specific PI3Kδ inhibitor(IC50=0.5 μM). |
| 细胞实验 | For AML cell proliferation assay, BMMCs are isolated and cultured in α-medium with 5% fetal calf serum (FCS) with or without FLT-3 ligand (10 ng/mL) for 48 hours and with or without IC87114. [3H]-thymidine (1 μCi [37 kBq]) is added for a final 6 hours and the amount of radioactivity incorporated is determined by trichloracetic acid precipitation. CD34+ cells from cord blood are cultured in stem cell factor (SCF; 20 ng/mL), FLT-3 ligand (10 ng/mL), and Tpo (20 nM) for 48 hours with or without 10 μM IC87114 and pulsed for 12 hours with [3H]-thymidine. (Only for Reference) |
| 激酶实验 | PI3K kinase assay: Phosphatidylinositol-(4,5)-bisphosphate (PIP2) containing phospholipid liposomes are prepared. Briefly, bovine PIP2 and phosphatidylserine (1:2 molar ratio) are vacuum-dried and resuspended at 1 mM PIP2 in 20 mM HEPES-KOH, pH 7.4, 50 mM NaCl, and 5 mM EDTA. The lipid suspension is subjected to a brief sonication, followed by 5 freeze-thaw cycles and then 20 extrusion cycles to produce the liposomes. The assay is conducted in 60 μL reaction volumes in 20 mM HEPES, pH 7.4, buffer containing 1 nM PI3K, 1 μM PIP2, 200 μM ATP, 1 μCi [γ-32P]ATP, 5 mM MgCl2, plus 50 μg/mL horse IgG as carrier protein. The reaction is incubated for 10 min at room temperature, quenched in 140 of 1 M K2PO4, 30 mM EDTA, pH 8.0, captured onto a 96-well polyvinylidene difluoride filter plate, and washed five times with 1 M K2PO4. The filter is allowed to dry completely, and the bound radioactivity is quantitated. IC87114 dilutions are assayed in a final concentration of 1% (w/w) DMSO. |
| 体外活性 | 在有炎症反应的鼠模型中,IC87114阻断TNF1α刺激产生蛋白酶的胞外分泌. |
| 体内活性 | 在人类中性粒细胞中,IC87114（5 μM）能够地抑制N-甲酰 - 甲硫氨酰 - 亮氨酰 - 苯丙氨酸（fMLP） - 刺激的磷脂酰肌醇三磷酸（PIP3）的生物合成和趋化性。在人类急性骨髓性白血病（AML）原始细胞如骨髓单个核细胞（BMMCs）中,IC87114（10 μM）抑制组成型和Flt-3刺激的Akt磷酸化和细胞增殖。在抗CD3刺激的小鼠CD62L +（幼稚）和CD62L-（效应/记忆）CD4 + T细胞中,IC87114抑制增殖和干扰素-γ（IFN-γ）产生。 |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 8 mg/mL (20.13 mM), Sonication is recommended.
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| 关键字 | Inhibitor | IC-87114 | inhibit | PI3K | IC87114 | Phosphoinositide 3-kinase |
| 相关产品 | (2S,3R,4S)-4-Hydroxyisoleucine | Quercetin Dihydrate | Apilimod | RLY-2608 | Bimiralisib | GDC0084 | Myricetin | 3-Methyladenine | Duvelisib (R enantiomer) hydrochloride | Isoprenaline hydrochloride | Erucic acid | Sapanisertib |
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